| Co-Investigator(Kenkyū-buntansha) |
OBIKA Satoshi Graduate School of Pharmaceutical Sciences, Osaka University, Assistant Professor, 薬学研究科, 助手 (80243252)
MIYASHITA Kazuyuki Graduate School of Pharmaceutical Sciences, Osaka University, Associate Professor, 薬学研究科, 助教授 (10166168)
DOI Takefumi Graduate School of Pharmaceutical Sciences, Osaka University, Professor, 薬学研究科, 教授 (00211409)
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| Research Abstract |
We studied the four subjects and obtained the results shown below:
(1) We have succeeded to synthesize 2'-0,4'-C-methylene bridged nucleic acid analogs (BNAs) and oligonucleotides containing the BNA (BNA-ODNs). The BNA-ODNs were found to have more effective duplex and triplex forming ability than natural ODNs and modified ODNs ever reported. Comparison of various properties of BNA-ODNs with those of natural ODNs and S-ODNs showed that the BNA-ODNs have an excellent antisense ability.
(2). We have designed and synthesized novel chiral vitamin B_6 model compounds having a chiral ansa-structure and/or a chiral ionophore structure, which were found to be effective for asymmetric α-alkylation ofα-amino esters and petides at the N-terminal position. Catalytic β-replacement reaction of a Ser derivative with thiols was also successfully achieved by employing the pyridoxal model compounds.
(3) We have synthesized fire-fly luciferin analogs having a heterocyclic structure in place of the benzothiazole structure of the fire-fly luciferin molecule, and studied their bioluminescent and chemiluminescent activities. As a result, it was found that the benzimidazole derivative shows effective light-emmisio by treatment with luciferase, while the benzoxazole derivative is effective for chemiluminescent induced by oxidative treatment.
(4) We have synthesized cationic lipid having a symmetrical structure, and studied gene transfection activity of liposome prepared from the lipid. As a consequence, it was found that the liposome composed of the symmetrical lipid, which was more easily prepared than that having an unsymmetrical structure, is low toxic and effective for gene transfection.
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